Name: | Amphotericin B |
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PubChem Compound ID: | 10533925 |
Description: | Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela. |
Molecular formula: | C47H73NO17 |
Molecular weight: | 964.778 g/mol |
Name: | Amphotericin B |
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Name (isomeric): | DB00681 |
Drug Type: | small molecule |
Description: | Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela. |
Synonyms: |
Amphotericine B; AMPH-B; Amphortericin B; Liposomal Amphotericin B
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Brand: | Abelcet, Amphotec, LNS-AmB, ABLC, SinuNase, Amphotericin, HSDB 3008 IAB, Fungisone, Fungizone Intravenous, Amphocin, IAB, Fungilin, Ampho-Moronal, AmB, Mysteclin-F, Fungizone, Tegopen, Halizon, AmBisome, Amphozone |
Category: | Anti-Bacterial Agents, Antiprotozoal Agents, Antifungal Agents, Amebicides |
CAS number: | 1397-89-3 |
Indication: | Used to treat potentially life threatening fungal infections. |
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Pharmacology: |
Amphotericin B shows a high order of in vitro activity against many species of fungi. Histoplasma capsulatum, Coccidioides immitis, Candida species, Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus are a...
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Mechanism of Action: |
Amphotericin B is fungistatic or fungicidal depending on the concentration obtained in body fluids and the susceptibility of the fungus. The drug acts by binding to sterols (ergosterol) in the cell membrane of susceptible fungi. This creates a transmembrane channel, and the resultant change in membrane permeability allowing leakage of intracellular...
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Absorption: | Bioavailability is 100% for intravenous infusion. |
Protein binding: | Highly bound (>90%) to plasma proteins. |
Biotransformation: | Exclusively renal |
Half Life: | An elimination half-life of approximately 15 days follows an initial plasma half-life of about 24 hours. |
Clearance: | 39 +/- 22 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day at Day 1] 17 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day 3-20 days later] 51 +/- 44 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day at Day 1] 22 +/- 15 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day 3-20 days later] 21 +/- 14 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day at Day 1] 11 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day 3-20 days later] |
Toxicity: | Oral, rat: LD50 = >5 gm/kg. Amphotericin B overdoses can result in cardio-respiratory arrest. |
Affected organisms: | Various Fungus Species |
Drug interaction: |
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